Abstract
Cissampelos pareira is significant medicinal plant of herbal materia medica. It is used in the
treatment of wide range of diseases in Traditional Chinese Medicine, Ayurevda and western herbalism.
The plant abounds in isoquinoline alkaloids; the chemicals that received a great deal of attention and
research in the late 1960. Antitumour potential of cissampareine and neuromuscular blocking effects of
hayatine are of special interest. The review summarizes ethno pharmacological investigations carried
out on the plant with special reference to isoquinoline alkaloids.
Keywords: Cissampelos pareira; isoquinoline alkaloids; pelosine; cissampareine; hayatine;
pharmacology
WayĂŁpi Indians use a decoction of the leaf and
stem as an oral analgesic (Gogte,2000).
Introduction
Cissampelos pareira Linn. is significant
India: In Ayurvedic system of medicine, the
plant of family Menispermaceae. There are 37
leaves are used in the treatment of indolent
plant species summarized under this botanical
ulcers (Kirtikar and Basu,2001) and diarrhea
name. Their taxonomic position is not clear. In
(Amresh et al.,2003). The plant is considered to
most cases, C. pareira or Pareira is used and the
be antiseptic and on account of this property, it
single species are called subspecies. It is found
is used in the treatment of urinary tract infection
in subtropical parts of India, Asia, East Africa
(Dandiya and Chopra,1970). Expressed juice of
and America (Singh,2005).
C. pareira is given in migraine (Singh,2005).
The plant is a climbing shrub, 2 - 5m
high with a thickened root. Leaves have an
Mexico: C. pariera has a long history of use for
orbicular shape 7-14 cm in diameter. They are
muscle inflammation, snakebite, rheumatism,
membranous or leathery, veined, glabrous to
diarrhea, dysentery, and menstrual problems
densely pilose. Flowers are green, male ones in
(Mokkhasmit,1971).
short umbels, 10 - 12cm long, females in
pendulous spikes, 7 - 10cm long, with a little
South America: C. pariera is commonly
round leaflet at the base of every flower (Prasad
referred to as the midwives' herb throughout
et al.,1962; Smitin and Larsen,1991).
South America. It ha been used for all types of
Traditional medicinal use
Brazil: C. pariera is widely employed in herbal
medicine today as a diuretic and as a tonic, as
well as to reduce fever and relieve pain. It is
often employed for menstrual cramps, difficult
menstruation, excessive bleeding and uterine
hemorrhages, fibroid tumors, pre- and postnatal
pain, colic, constipation, poor digestion, and
dyspepsia (Mukerji and Bhandari,1959; Feng et
al.,1962).
French Guyana: The roots are used in the
treatment of dysuria and renal calculi. The

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women's ailments. The root is used in tropical
countries to prevent a threatened miscarriage and
to stop uterine hemorrhages after childbirth.
Midwives in the Amazon still carry abuta with
them for menstrual cramps and pre- and
postnatal pain, excessive menstrual bleeding,
and uterine hemorrhaging (Floriani,1936).
Thailand: The extract from its leaves can be
used to make gel. The dark green gel is used as
medicine for treating fever in local people. Local
people use this plant as a diuretic and for the
treatment of a variety of ailments, including

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International Journal of Biological Technology (2010) 1(1):114-120

asthma and for traumas (Mokkhasmit et
al.,1971).
Phytochemistry: An amorphous, white alkaloid,
pelosine (Figure 1) was studied in association
with
an
indifferent body, deyamittin.
Cissampelosine was reported from C. pariera
which was later on shortened as pelosine
(Wiggers, 1838).
CH3
CH3

N

O

O

(++)-4 -O-methylcurine (Fig. 3), a new alkaloid
was isolated from C. pareira (Haynes et
al.,1966).
l-curine
(Fig.4),
d-isochondrodendrine (Fig.5), and hayatine (Fig.6)
were isolated from the roots and vines of C.
pareira from Madras (Kupchan et al.,1966).
Preliminary pharmacological study of the
methanol-extractable
alkaloids,
of
the
methiodide prepared from the latter mixture, and
of the quaternary alkaloids, showed that all had
curare-like
activity
(Mukerji
and
Bhandari,1959).
O

O

N
O

O

O

O
N

CH3

N
O

HO

CH3

Fig. 3: Structure of (++)-4”-O-Methylcurine

Fig.1: Structure of Pelosine

OH

Eleven years later, studies on pelosine
and bebeerine were undertaken and both the
alkaloids were proved to be different
(Bodeker,1849). However a study proved
similarity with the alkaloids bebeerine and
buxine (Flückiger,1869). A comparative analysis
of C. pareira demonstrated presence of starch,
gum, tannin, phlobaphene, and an alkaloid
(Ringer and Brooke, 1982).

O

O
H

N

O
N
N

O

OH
O

HO
O

C. pareira contain a group of plant
chemicals called isoquinoline alkaloids (Roy et
al.,1959). Since the late 1960s, these chemicals
have received a great deal of attention and
research (Boissier et al.,1965). Cissampareine
(Figure 2) was reported from C. pareira growing
in Peru (Kupchan,1964). Cissampareine was
found to show significant and reproducible
inhibitory activity against human carcinoma of
the nasopharynx carried in cell culture (KB).
Cissampareine is isomeric with methylwarifteine
found in dried rhizomes of C. ovalifolia DC.
CH3
N

Tetrandrine (Fig.13) has been reported from the
roots of C. pareira growing in Thailand
(Rojanasonthorn,1970). Dicentrine (Fig.14),
dihydrodicentrine,
cycleanine,
insularine
(Fig.15) and isochondrodendrine have been
reported from roots of the plant growing in
Ghana (30). Isolation of pareirubrine A (Fig.16)
and B (Fig. 17), novel tropoloisoquinoline
alkaloids with antileukemic activity has been
reported (Morita et al.,1993).
CH3

Tropoloisoquinoline alkaloid pareitropone (Fig.
18) has been reported (Morita et al.,1993). A
novel azafluoranthene alkaloid, norimeluteine
(Fig.19), has been isolated as a cytotoxic
substance from C. pareira together with an
alkaloid having the same skeleton, norruffscine
(Morita et al.,2002).

OH
OH
CH3
O

O

CH3

O
H3C

O

N

Fig. 23: Structure of grandirubrine

H3CO

N

H3CO
H3C

CH3
O
O

HO

CH3

N
O
CH3

Fig.18:Structure of Pareitropone
Fig. 19. Structure of Norimeluteine
An antiprotozoal chalcone-flavone
dimer, cissampeloflavone (Fig.21) has been
isolated from the aerial parts of C. pareira. It has
good activity against Trypanosoma cruzi and T.
brucei rhodesiense and has a low toxicity to the

dose dependent anti-inflammatory activity in the
carrageenin test, which was based on
interference with prostaglandin synthesis, as
confirmed by the arachidonic acid test. In the
abdominal writhing test induced by acetic acid,
higher dose of the plant extract had the highest
analgesic activity, whereas in the hot-plate test
the best dose was 100 mg/kg (p< 0.05). The
LD50 showed that C. pareira (2000 mg/kg)
presented low toxicity (Amresh et al.,2007).
In yet another study, 50% ethanolic
extract of C. pareira roots in acute, subacute and
chronic models of inflammation was assessed in
rats. Per os (p.o.) administration of C. pareira
(200, 400 mg/kg) exhibited significant antiinflammatory activity. In acute inflammation as
produced by carrageenin 59.55% and 64.04%,
by histamine 15.38% and 30.77%, by 5hydroxytryptamine 17.78% and 31.11% and by
prostaglandin E2-induced hind paw edema
19.23% and 30.77% protection was observed.
While in subacute anti-inflammatory models
using formaldehyde-induced hind paw edema
(after 1.5 h) 38.36% and 47.95% and in chronic
anti-inflammatory model using cotton pellet
granuloma 15.02% and 19.19% protection from
inflammation was observed (Amresh et
al.,2008).
Antifertility activity: C. pareira leaf extract,
when administered orally, altered the estrous
cycle pattern in female mice, prolonged the
length of estrous cycle with significant increase
in the duration of diestrus stage and reduced
significantly the number of litters in albino mice.
The analysis of the principal hormones involved
in estrous cycle regulation showed that the plant
extract altered gonadotropin release (LH, FSH
and prolactin) and estradiol secretion. The oral
LD50 of the extract was found to be 7.3 g/kg in
mice. (Ganguly et al.,2007)
Antioxidant activity: C. pareira extract showed
significant antioxidant activity in the 1,1 diphenyl-2-picrylhydrazyl assay. C. pareira
extract was found to significantly scavenge
superoxide, hydrogen peroxide, hydroxyl
radicals, and nitric oxide at a dose regimen of 50
to 400 Âľg/kg in vitro. C. pareira extract also
inhibited hydroxyl radical-induced oxidation of
proteins in vitro. C. pareira extract exhibit a
potent protective activity in an acute oxidative
tissue injury animal model: benzo (a) pyreneinduced gastric toxicity in mice in vivo (Amresh
et al.,2007).

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Chemo preventive effects: The protective effect
of C. pareira extract was studied against benzo
(a) pyrene [B(a)P]-induced gastric cancer in
mice, and the tumor incidence was reduced and
the mean number of tumors and the tumor
multiplicity were reduced significantly and dosedependently. The modulatory effect of C.
pareira extract was also examined on carcinogen
metabolizing phase I and phase II enzymes,
antioxidant enzymes, glutathione content, lactate
dehydrogenase, and lipid peroxidation in liver.
Significant increases in the levels of acid-soluble
sulfhydryl (-SH) and cytochrome P450 contents
and in enzyme activities of cytochrome P450
reductase, cytochrome b5 reductase, GST, DTD,
SOD, catalase, glutathione (GSH) peroxidase,
and
GSH
reductase
but
decreased
malondialdehyde (MDA) were observed.
(Amresh et al.,2007)
Anti-hemorrhagic effects: To establish the antihemorrhagic activity of aqueous extract from
leaves of C. pareira, the skin of mice was
injected with a mixture of extract and venom,
and it as found that extract produced a total
inhibition of this activity. On the other hand,
experiments regarding the anti-proteolytic
activity were conducted observing the effect on
casein in a test tube or on biotinylated casein in a
microplate. None of the two procedures was able
to show any inhibitory activity (Badilla et
al.,2008).
Toxicity
In the acute toxicity test, oral
administration of 2 g/kg of C. pareira produced
neither mortality nor changes in behavior or any
other physiological activities in mice. In
subacute toxicity studies, no mortality was
observed when the two doses of 1 or 2 g/kg day
of 50% aqueous ethanolic extract of C. pareira
were administered p.o. for a period of 28 days in
rats. There were no significant changes occurred
in the blood chemistry analysis in both sexes of
animals. Hematological analysis showed no
marked differences in any of the parameters
examined in either the control or treated group
of both sexes. Pathologically, neither gross
abnormalities nor histopathological changes
were observed (Amresh et al.,2008).
Pharmacology of hayatine
Hayatin methiodide has been used as a
muscle relaxant during surgery in 100 patients.
This drug provided adequate relaxation for
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International Journal of Biological Technology (2010) 1(1):114-120

endotracheal intubation and surgery. It appeared
to be about one-third as potent as tubocurarine.
The duration of both these drugs was of equal
magnitude
in
equipotent
doses.
The
neuromuscular block produced by this drug
could be completely reversed by neostigmine. It
was relatively free from serious side-effects and
appears to be a promising muscle relaxant.